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Ketoconazole tablets

Function and Efficacy

Ketoconazole is a synthetic imidazole dioxane derivative that has antibacterial and bactericidal activity against dermatophytes, yeasts (Candida, Pityrosporum, Torulopsis, Cryptococcus), dimorphic fungi and fungi. Ketoconazole is less sensitive to Aspergillus, Sporothrix schenckii, some dematiaceae, and Mucor, but is an exception to Entomophthorales. Ketoconazole inhibits the biosynthesis of fungal ergosterol and changes the composition of other lipid compounds in the cell membrane. Long-term animal toxicity experiments have shown that this product can significantly increase alkaline phosphatase and degenerate liver cells.

Ingredients

The main chemical component is ketoconazole, whose chemical name is 1-acetyl-4[4-[2-(2,4-dichlorophenyl)-2(1H-imidazole-1-methyl)-1,3-dioxolane-4-methoxy]phenyl]-piperazine.

Name Description Content CAS NO. Manufacturer
KetoconazoleIngredients

Synthetic imidazole dioxane derivatives have antibacterial and bactericidal activities against dermatophytes, yeasts (Candida, Pityrosporum, Torulopsis, Cryptococcus), dimorphic fungi and fungi. It inhibits the biosynthesis of ergosterol in fungi and changes the composition of other lipid compounds in cell membranes. Long-term animal toxicity experiments have shown that this product can significantly increase alkaline phosphatase and degenerate liver cells.

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65277-42-1 25

Appearance

This product is white tablets.

Indication

Systemic fungal infections, such as systemic candidiasis, paracoccidioidomycosis, and histoplasmosis. This drug can be used to treat infections of the skin, hair, and nails (dermatophytes, onychomycosis, perionychia, tinea versicolor, chronic skin and mucosal candidiasis, etc.) caused by dermatophytes and/or yeasts when local treatment is ineffective or it is difficult to apply the drug due to factors such as the site, area, and depth of infection. Gastrointestinal yeast infections. Chronic and recurrent vaginal candidiasis that is ineffective with local treatment. Used for the prevention and treatment of patients who are susceptible to fungal infections due to reduced immune function (hereditary and caused by disease or drugs). This product has poor penetration into the central nervous system and is not suitable for the treatment of fungal meningitis.

Usage and Dosage

This product must be used under the guidance of a doctor. Adults: Deep fungal infection: Oral, 1-2 times a day, 1 tablet (200 mg) each time. Skin infection: Oral, 1 tablet (200 mg) once a day, taken with meals. If necessary, it can be increased to 1 time a day, 2 tablets (400 mg) each time, or 2 times a day, 1 tablet (200 mg) each time. Vaginal candidiasis: Oral, 1 time a day, 2 tablets (400 mg) each time, taken with meals. Children: Deep fungal infection: Oral, 4-8 mg per kilogram of body weight per day. Skin infection: Children weighing less than 15 kg, 3 times a day, 20 mg each time; children weighing 15-30 kg, 1 time a day, 1/2 tablet each time, or as directed by a doctor. Children weighing more than 30 kg, the same as adults. Preventive treatment of immunodeficient patients: Adults: 2 tablets (400 mg) per day. Children: 4-8 mg per kilogram of body weight per day.

Adverse Reactions

Some patients experience gastrointestinal discomfort, nausea, headache, dizziness, photophobia, paresthesia, and thrombocytopenia. Drug rash, itching, and hair loss are occasionally seen, and a few patients have reported allergic reactions. Liver damage may occur in a very small number of patients (mostly with idiosyncratic constitutions). This reaction often occurs in patients with a history of liver disease or drug sensitivity, and generally recovers after timely discontinuation of the drug. When the therapeutic dose exceeds the recommended daily 200 mg or 400 mg, reversible gynecomastia and lack of semen may occur in rare cases. When taken at a dose of 200 mg once a day, there are occasional reports of hair loss, and a temporary decrease in plasma testosterone concentration may also occur, but the plasma testosterone concentration will return to normal within 24 hours after taking the drug. When this dose is used for long-term treatment, the amount of testosterone is not much different from that of the control group.

Precautions

This product is contraindicated in patients with acute or chronic liver disease or patients with known allergy to this product.

Special Population Medication

Precautions for children: There is limited information on the use of this product in children weighing less than 15kg, so it is not recommended for children. Precautions for pregnancy and lactation: Pregnant women have limited experience with the use of this product. Animal studies have shown that this product is reproductively toxic. The potential risks of human use are unknown. Therefore, this product should not be used during pregnancy unless the potential benefit to the mother outweighs the potential risk to the fetus. This product can be excreted in breast milk during lactation, so lactating women should stop breastfeeding when taking this product. Precautions for the elderly: Use with caution in elderly patients.

Drug Interactions

Since the absorption of this product depends on sufficient gastric secretion, it should be avoided to take it at the same time with drugs that inhibit gastric secretion (such as anticholinergics, antacids, H2 receptor antagonists, etc.). If you need to take these drugs at the same time, you should take them at least 2 hours apart. Taking rifampicin, isoniazid and ketoconazole at the same time can reduce the blood concentration of the latter, so they should not be taken at the same time. Since ketoconazole inhibits certain liver oxidative enzymes, it can reduce the clearance of drugs that rely on this enzyme metabolism. If such drugs are taken with this product, the blood concentration of the former may increase and the side effects may also be aggravated. Case reports have shown that ketoconazole can have serious interactions with cyclosporine, terfenadine, anticoagulants, methylprednisolone and myleran. If these drugs need to be taken with this product, the dosage should be reduced. Occasionally, there are case reports that this product has a disulfiram-like effect on drinkers, manifested as flushing, rash, peripheral edema, nausea and headache, which can completely disappear within a few hours. Patients treated with griseofulvin should stop taking the drug for one month before starting this product.

Storage

Store in a dry place at 15-30℃ and out of reach of children.

Packaging Specification

0.2g*10s

Validity Period

36 months

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